ChemicalBook > CAS DataBase List > BIIB-021

BIIB-021

Product Name
BIIB-021
CAS No.
848695-25-0
Chemical Name
BIIB-021
Synonyms
CS-479;CNF2024;BIIB-021;CNF-2024EC102;BIIB021 ，S1175;BIIB021/CNF2024;BIIB 021, ≥98%;BIIB021 BIIB-021;BIIB-021 USP/EP/BP;CNF 2024 - BIIB 021
CBNumber
CB62516264
Molecular Formula
C14H15ClN6O
Formula Weight
318.76
MOL File
848695-25-0.mol
More
Less

BIIB-021 Property

Melting point:
192-193℃
Boiling point:
588.5±60.0 °C(Predicted)
Density 
1.50
storage temp. 
-20°C
solubility 
Soluble in DMSO (>25 mg/ml)
pka
6.07±0.40(Predicted)
form 
solid
color 
White
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 montha.
InChI
InChI=1S/C14H15ClN6O/c1-7-4-17-9(8(2)11(7)22-3)5-21-6-18-10-12(15)19-14(16)20-13(10)21/h4,6H,5H2,1-3H3,(H2,16,19,20)
InChIKey
QULDDKSCVCJTPV-UHFFFAOYSA-N
SMILES
N1C2C(=NC(N)=NC=2Cl)N(CC2=NC=C(C)C(OC)=C2C)C=1
More
Less

Safety

HS Code 
2921490090
More
Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

More
Less

N-Bromosuccinimide Price

Cayman Chemical
Product number
18269
Product name
BIIB021
Purity
≥98%
Packaging
1mg
Price
$25
Updated
2024/03/01
Cayman Chemical
Product number
18269
Product name
BIIB021
Purity
≥98%
Packaging
5mg
Price
$50
Updated
2024/03/01
Cayman Chemical
Product number
18269
Product name
BIIB021
Purity
≥98%
Packaging
10mg
Price
$88
Updated
2024/03/01
Cayman Chemical
Product number
18269
Product name
BIIB021
Purity
≥98%
Packaging
25mg
Price
$156
Updated
2024/03/01
Tocris
Product number
4608
Product name
BIIB021
Purity
≥98%(HPLC)
Packaging
10
Price
$219
Updated
2021/12/16
More
Less

BIIB-021 Chemical Properties,Usage,Production

Description

BIIB021 is a potent HSP90 inhibitor (IC50 = 30 nM HER-2 degradation).1 It inhibited the proliferation of MCF7 and BT474 breast cancer cell lines (IC50 = 100 nM for each).? BIIB021 has shown efficacy as a therapeutic in multiple cancer models.2-5

Uses

BIIB 021 an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90. Studies show that BIIB 021 adminisitration led to degradation of Hsp90 client proteins measured in tumor tissue and resulted in the inhibition of tumor growth in several human tumor xenograft models.

Definition

ChEBI: A member of the class of 2-aminopurines that is 2-aminopurine which is substituted by a chlorine at position 6 and by a (4-methoxy-3,5-dimethylpyridin-2-yl)methyl group at position 9.

Synthesis

86604-75-3

10310-21-1

848695-25-0

The general procedure for the synthesis of 6-chloro-9-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-9H-purin-2-amine (BIIB021) from 2-chloromethyl-3,5-dimethyl-4-methoxypyridine hydrochloride and 2-amino-6-chloropurine was as follows: 1. 2-Amino-6-chloropurine (10 mmol) and anhydrous potassium carbonate (12 mmol) were weighed separately and added to 25 mL of DMSO in a 50 mL round bottom flask. 2. The reaction mixture was heated to 48°C in an oil bath with continuous stirring for 30 minutes. 3. 2-chloromethyl-3,5-dimethyl-4-methoxypyridine hydrochloride (11 mmol) was weighed and added to the above reaction solution in 3 portions at 30 minute intervals. 4. After continuing the reaction at 48°C for 10 hours, the reaction temperature was adjusted to 22°C and stirred for 2 hours. 5. Upon completion of the reaction, the reaction mixture was filtered and the filtrate was retained. 6. A mixture of water and isopropanol (1:1 by volume) was added slowly and dropwise to the filtrate until the solution became turbid. 7. Place the turbid solution in a refrigerator overnight. 8. Collect the precipitate by filtration to obtain the target product BIIB021. The product 6-chloro-9-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-9H-purin-2-amine (BIIB021) was a pale yellow solid with 77% yield.

in vivo

Oral administration of BIIB021 leads to tumor growth inhibition in many tumor xenograft models including N87, BT474, CWR22, U87, SKOV3 and Panc-1[1]. BIIB021 effectively inhibits growth of L540cy tumor at a dose of 120 mg/kg[2]. BIIB021 significantly enhances antitumor growth effect of radiation in JHU12 xenograft[3].

IC 50

HSP90: 1.7 nM (Ki); HSP90: 38 nM (EC50)

References

[1] SRINIVAS R. KASIBHATLA. Rationally Designed High-Affinity 2-Amino-6-halopurine Heat Shock Protein 90 Inhibitors That Exhibit Potent Antitumor Activity[J]. Journal of Medicinal Chemistry, 2007, 50 12: 2767-2778. DOI:10.1021/jm050752+
[2] KAREN LUNDGREN. BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90.[J]. Molecular Cancer Therapeutics, 2009: 921-929. DOI:10.1158/1535-7163.mct-08-0758
[3] BORIS BÖLL. Heat shock protein 90 inhibitor BIIB021 (CNF2024) depletes NF-kappaB and sensitizes Hodgkin’s lymphoma cells for natural killer cell-mediated cytotoxicity.[J]. Clinical Cancer Research, 2009: 5108-5116. DOI:10.1158/1078-0432.ccr-09-0213
[4] HONG ZHANG. BIIB021, a synthetic Hsp90 inhibitor, has broad application against tumors with acquired multidrug resistance[J]. International Journal of Cancer, 2009, 126 5: 1226-1234. DOI:10.1002/ijc.24825
[5] XIN-TONG WANG . BIIB021, a novel Hsp90 inhibitor, sensitizes esophageal squamous cell carcinoma to radiation[J]. Biochemical and biophysical research communications, 2014, 452 4: Pages 945-950. DOI:10.1016/j.bbrc.2014.09.026

BIIB-021 Preparation Products And Raw materials

Raw materials

Preparation Products

More
Less

BIIB-021 Suppliers

Canada 1 China 139 India 3 Japan 1 United Kingdom 2 United States 21 Global 167
Beijing Yisiyan Technology Research Center
Tel
010-56645598 13366904824
Fax
01062230033
Email
bjkaida@163.com
Country
China
ProdList
1618
Advantage
59
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
J & K SCIENTIFIC LTD.
Tel
18210857532; 18210857532
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
Advantage
76
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6003
Advantage
61
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
16075
Advantage
64
Chemsky (shanghai) International Co.,Ltd
Tel
021-50135380
Email
shchemsky@sina.com
Country
China
ProdList
15402
Advantage
60
Jinan Trio PharmaTech Co., Ltd.
Tel
0531-88811783
Fax
+86 (531) 55696010 QQ 1762738062
Email
sales@trio-pharmatech.com
Country
China
ProdList
1856
Advantage
62
BOC Sciences
Tel
1-631-485-4226; 16314854226
Email
info@bocsci.com
Country
United States
ProdList
12952
Advantage
65
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4747
Advantage
58
Shanghai civi chemical technology co.,Ltd
Tel
86-21-34053660
Fax
86-21-34053661
Email
sale@labgogo.com
Country
China
ProdList
9865
Advantage
52
More
Less

View Lastest Price from BIIB-021 manufacturers

Henan Aochuang Chemical Co.,Ltd.
Product
BIIB-021 848695-25-0
Price
US $0.00-0.00/KG
Min. Order
1KG
Purity
98%
Supply Ability
1Ton
Release date
2022-10-13

848695-25-0, BIIB-021Related Search:

NOTUMib-1 AZ20 BI 2536 Imiquimod PU-H71 Onalespib PD 0332991 HCl 17-AAG Ganetespib Olaparib

  • CNF2024
  • 9-[2-(2,2-diMethyl-propylaMino)ethyl]-8-(2-iodo-5-Methoxy-phenylsulfanyl)-9H-purin-6-ylaMine
  • CNF-2024EC102
  • 9H-Purin-2-aMine, 6-chloro-9-[(4-Methoxy-3,5-diMethyl-2-pyridinyl)Methyl]-
  • 6-chloro-9-((4-Methoxy-3,5-diMethylpyridin-2-yl)Methyl)-9H-purin-2-aMine
  • BIIB-021
  • BIIB021/CNF2024
  • 6-Chloro-9-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-9H-purin-2-amine
  • 6-CHLORO-9-[(4-METHOXY-3,5-DIMETHYLPYRIDIN-2-YL)METHYL]PURIN-2-AMINE
  • 6-Chloro-9-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-9H-purin-2-amine BIIB 021
  • BIIB 021 6-Chloro-9-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-9H-purin-2-amine
  • BIIB021(CNF2024)BIIB021
  • BIIB 021 (This product is only available in Japan.)
  • BIIB021;BIIB-021; BIIB 021
  • CNF 2024 - BIIB 021
  • CNF2024; BIIB-021; BIIB 021; CNF 2024; CNF-2024
  • CS-479
  • BIIB-021 USP/EP/BP
  • BIIB 021, ≥98%
  • BIIB021 BIIB-021
  • BIIB021, 10 mM in DMSO
  • BIIB021 ，S1175
  • 6-Chloro-9-((3,5-dimethyl-4-methoxy-pyridin-2-yl)methyl)-9H-purin-2-ylamine
  • 848695-25-0
  • C14H15ClN6O
  • Aromatics
  • Heterocycles
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Antineoplastic
  • Inhibitor